盐酸吉西他滨的合成  

Synthesis of Gemcitabine Hydrochloride

作　　者：王英华[1] 王星海[1] 仇缀百[1] 

机构地区：[1]复旦大学药学院,上海200032

出　　处：《中国医药工业杂志》2007年第4期249-251,共3页Chinese Journal of Pharmaceuticals

摘　　要：2-脱氧-2,2-二氟-D-赤型-呋喃戊糖-1-酮-3,5-二苯甲酸酯经四氢锂铝还原、甲磺酰化得2-脱氧-2,2-二氟-D-呋喃核糖-3,5-二苯甲酸酯-1-甲磺酸酯,与胞嘧啶缩合后在含氨甲醇中脱保护基,成盐后于含水丙酮中结晶分离得盐酸吉西他滨,总收率14%。Gemcitabine hydrochloride was prepared from 2-deoxy-2,2-difluoro-D-erythro-pentofuranose-1- ketose-3,5-dibenzoate via LiAlH4 reduction and methylsulfonation to afford 2-deoxy-2,2-difluoro-D-ribofuranose-3,5- dibenzoate-1-methylsulfonate （3α/β）, which was subjected to condensation with cytosine followed by deprotection, salt formation and separative crystallization in aqueous acetone with an overall yield of 14 %.

关 键 词：盐酸吉西他滨 抗肿瘤药 合成 

分 类 号：R971[医药卫生—药品]